| Identification | Back Directory | [Name]
R-121,919 | [CAS]
195055-03-9 | [Synonyms]
R-121,919
NBI 30775
R121919 (NBI-30775)
-4-methylpyridin-3-yl)
NBI30775;R 121919;R-121919
-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine
3-(6-(Dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7
3-(6-(Dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-am
3-[6-(DiMethylaMino)-4-Methyl-3-pyridinyl]-2,5-diMethyl-N,N-dipropylpyrazolo[1,5-a]pyriMidin-7-aMine
3-(6-(DIMETHYLAMINO)-4-METHYLPYRIDIN-3-YL)-2,5-DIMETHYL-N,N-DIPROPYLPYRAZOLO[1,5-A]PYRIMIDIN-7-AMINE
3-[6-(diMethylaMino)-4-Methyl-3-pyridinyl]-2,5-diMethyl-N,N-dipropyl-pyrazolo[2,3-a]pyriMidine-7-aMine
Pyrazolo[1,5-a]pyrimidin-7-amine, 3-[6-(dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropyl- | [Molecular Formula]
C22H32N6 | [MDL Number]
MFCD05260874 | [MOL File]
195055-03-9.mol | [Molecular Weight]
380.53 |
| Chemical Properties | Back Directory | [density ]
1.11±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 6.2 mg/mL (16.29 mM) | [form ]
Solid | [pka]
6.33±0.10(Predicted) | [color ]
White to off-white | [InChI]
1S/C22H32N6/c1-8-10-27(11-9-2)20-13-16(4)24-22-21(17(5)25-28(20)22)18-14-23-19(26(6)7)12-15(18)3/h12-14H,8-11H2,1-7H3 | [InChIKey]
ANNRUWYFVIGKHA-UHFFFAOYSA-N | [SMILES]
CCCN(CCC)C1=CC(C)=NC2=C(C(C)=NN12)C3=CN=C(C=C3C)N(C)C |
| Hazard Information | Back Directory | [Uses]
3-[6-(Dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine, is a potent and Orally active Corticotropin-Releasing factor 1 receptor antagonists, which is hown to reduce negative emotional symptoms of acute and protracted alcohol withdrawal, and thus used for the treatment of alcoholism. | [Biological Activity]
R121919 (NBI 30775) is a brain-penetrantorally available high-affinity corticotropin-releasing factor/hormone (CRF or CRH) receptor 1 (CRF1CRF-R1CRFR-1CRH-R1CRHR-1) antagonist (Ki = 3.5 nM against sauvagine for binding hCRFR1-expressing HEK293 cells; IC50 = 20 nM/CRF-stimulated ACTH release from r at anterior pituitary cells & IC50 = 80 nM/CRF-stimulated cAMP production in hCRFR1-expressing HEK293 cells) without affinity toward CRFR2. In addition to its antistress efficacy in various r at anxiety models (0.63-20 mg/kg p.o.)R121919 also demonstrates therapeutic efficacy and long-term safety in Alzheimerμs disease (AD) mice (20 mg/kg/day s.c.) in vivo. | [in vivo]
R121919 (NBI30775) dose dependently decreases adrenocorticopin hormone and Corticosterone (HY-B1618) responses to restraint stress in rats. Peak plasma adrenocorticopin hormone and corticosterone concentrations at a dose of 10 mg/kg R121919 are 9 and 25%, respectively[1].
R121919 reduces levels of anxiety in mice with a steep dose-response curve[2]. | [IC 50]
CRFR1: 2-5 nM (Ki) | [storage]
Store at -20°C |
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